Drug Metabolism in Drug Design and Development Basic Concepts and Practice

Mass analyzers, 325 329
beam-type, 325
ion-trapping, 325
Mass balance, 586
Mass defect filter (MDF), 346, 348, 584
Mechanism-based inhibition, (MBI), 526
kinetic model, 528
Membrane-based assays, 176
Metabolic activation, 448
pathways, 319, 346, 447
Metabolite in safety testing (MIST), 208,
273, 574
Metabolite profiling, 245, 270, 583, 591
analytical methods, 213
Michaelis–Menten equation, 90, 91, 103
Michaelis–Menten kinetics, 90, 425, 514
Microarray technology, 532
Microplate scintillation counting (MSC),
583
Ministry of Health, Labor and Welfare
in Japan (MHLW), 209
Mitoxantrone resistance protein (MXR),
138
Monoamine oxidase (MAO), 22, 482
Multidrug resistance-associated proteins
(MRP), 225
Multiple reaction-monitoring (MRM), 521
Myelodysplastic syndrome (MDS), 155
Myeloperoxidase, 246

N-acetyltransferases (NATs), 484
NADPH-P450 reductase, 27
Nanospray ionization (NSI), 343
New chemical entities (NCEs), 116,
413, 448, 478, 513
New drug application (NDA), 210, 281
New radiochromatography techniques,
293
NMR (1D), 381, 383
Chemical shifts, 375, 377
Coupling constants, 378
NOE, 382, 383
Water suppression, 385, 397
NMR hardware, 372
NMR spectroscopy, 5, 348, 380, 381
NMR spectrum, 373, 381
Noncompetitive inhibition, 104
Noncytochrome p450 reaction
phenotyping, 481

Nonsteroidal anti-inflammatory drugs

(NSAIDs), 172

Northern blot, 554, 555

Nuclear magnetic resonance (NMR), 369

Nuclear overhauser experiment (NOE),

382

Nuclear receptors (NRs), 122

Nucleotide binding domains (NBDs), 138

Online radiochromatographic technique,

298, 308

Online radioflow detection (RFD), 290

Oral therapy, 239

Organic anion transporter (OAT), 225

Organic anion transporting polypeptide

(OATP), 225

Organic cation transporter (OCT), 225

Paraoxonases (PON), 483

Parkinson’s disease-type syndrome, 22

Peroxidases, 24, 25

Peroxisome proliferator-activated

receptor (PPAR), 54

Pharmaceutical Research

and Manufactures of America

(PhRMA), 514

Pharmacodynamic (PD) inhibition, 513

Pharmacokinetic optimization, 8

Phenacetin metabolic pathways, 251

Plasma concentration–time curve,

438, 588

Polycyclic aromatic hydrocarbon (PAH),

28

Precursor ion scan (PIS), 329

Pregnane X receptor (PXR), 181

Probenecid, 60

PXR-dependent induction pathway, 553

PXR reporter gene assays, 557, 560, 562

Quadrupole ion trap (QIT), 327

Quadrupole mass analyzer, 326

Quantitative whole body autoradiography

(QWBA), 268

Quinone reductase (NQO), 28

Radioactive isotopes, 289

Radioactivity recovery determination, 298

Radiochromatography techniques, 290, 293

Radiolabeled drugs, 575

608 INDEX